Synthesis of novel forskolin isoxazole derivatives with potent anti-cancer activity against breast cancer cell lines

被引：34
|
作者：
Burra, Srinivas [1 ]
Voora, Vani [2 ]
Rao, Ch. Prasad [1 ]
Kumar, P. Vijay [1 ]
Kancha, Rama Krishna [2 ]
Krupadanam, G. L. David [1 ]
机构：
[1] Osmania Univ, Dept Chem, Nat Prod Lab, Hyderabad 500007, Andhra Pradesh, India
[2] Osmania Univ, Mol Med & Therapeut Lab, CPMB, Hyderabad 500007, Andhra Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 18期
关键词：
Forskolin; Isoxazoles; Breast cancer; 1,3-Dipolar cycloadditions; Regioselectivity; 1,3-DIPOLAR CYCLOADDITIONS; CARCINOMA CELLS; DOXORUBICIN; RESISTANT; INHIBITION; FORMESTANE; EXEMESTANE; LETROZOLE; ACTIVATOR; ANALOGS;
D O I：
10.1016/j.bmcl.2017.08.033
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Forskolin C-1-isoxazole derivatives (3,5-regioisomers) (11a-e, 14, 15a-h and 15, 16a-g) were synthesized regioselectively by adopting 1,3-dipolar cycloadditions. These derivatives were tested using estrogen receptor positive breast cancer cell lines MCF-7 and BT-474. Majority of the compounds exhibited activity against the p53-positive MCF-7 breast cancer cells but not against the p53-negative BT-474 breast cancer cells. Among forskolin derivatives, compounds 11a, 11c, 14a, 14f, 14g, 14h, 15b, 16g and 17b exhibited higher anti-cancer activity against MCF-7 cell line with an IC50 <= 1 mu M. The derivative 14f exhibited highest activity in both p53-positive (MCF-7) and p53-negative (BT-474) breast cancer cell lines with an IC50 of 0.5 mu M. (C) 2017 Published by Elsevier Ltd.
引用
收藏
页码：4314 / 4318
页数：5
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